Butterfield D A, Rangachari A
Department of Chemistry, University of Kentucky, Lexington 40506-0055.
Life Sci. 1993;52(3):297-303. doi: 10.1016/0024-3205(93)90221-n.
Electron paramagnetic resonance has been used to investigate the effects of interaction of acetylcarnitine with cytoskeletal proteins in human erythrocyte membranes. This compound, currently in clinical trials as a potential therapeutic agent for Alzheimer's disease, caused a highly significant increase in cytoskeletal protein-protein interactions. Carnitine, the parent compound, also increased cytoskeletal protein-protein interactions, suggesting that the acetyl group is not hydrophobic enough to direct acetylcarnitine to the bilayer phase of the membrane. Consistent with this suggestion, no change in lipid order or dynamics with acetylcarnitine was observed. These results are discussed in terms of possible implications to Alzheimer's disease treatment.
电子顺磁共振已被用于研究乙酰肉碱与人红细胞膜细胞骨架蛋白相互作用的影响。这种目前正处于作为阿尔茨海默病潜在治疗剂临床试验阶段的化合物,导致细胞骨架蛋白 - 蛋白相互作用显著增加。其母体化合物肉碱也增加了细胞骨架蛋白 - 蛋白相互作用,这表明乙酰基团的疏水性不足以将乙酰肉碱导向膜的双层相。与这一推测一致,未观察到乙酰肉碱对脂质有序性或动力学的影响。根据这些结果对阿尔茨海默病治疗的可能意义进行了讨论。